Abstract: Disclosed is a method for production of an optically active biphenylalanine compound represented by the formula (2): (wherein, R2 is a protective group of an amino group, and R3 and R4 are each independently a hydrogen atom, etc.) or a salt thereof and an optically active biphenylalanine ester compound represented by the formula (3): (wherein, R1 is an alkyl group, etc.) wherein the method comprises hydrolyzing a biphenylalanine ester compound represented by the formula (1): with a protease produced by a microorganism belonging to Bacillus sp. in the presence of at least one alkali selected from an alkali metal hydroxide and an alkaline earth metal hydroxide.

Abstract: Disclosed is a method for production of an optically active biphenylalanine compound represented by the formula (2): (wherein, R2 is a protective group of an amino group, and R3 and R4 are each independently a hydrogen atom, etc.) or a salt thereof and an optically active biphenylalanine ester compound represented by the formula (3): (wherein, R1 is an alkyl group, etc.) wherein the method comprises hydrolyzing a biphenylalanine ester compound represented by the formula (1): with a protease produced by a microorganism belonging to Bacillus sp. in the presence of at least one alkali selected from an alkali metal hydroxide and an alkaline earth metal hydroxide.

Abstract: The present invention provides a process for producing 4-(2-methylphenyl)benzotrifluoride, comprising reacting 4-chlorobenzotrifluoride with 2-methylphenylmagnesium chloride in the presence of cobalt-based catalyst and zinc salt.

Abstract: The present invention provides a process for producing 4-(2-methylphenyl)benzotrifluoride, comprising reacting 4-chlorobenzotrifluoride with 2-methylphenylmagnesium chloride in the presence of cobalt-based catalyst and zinc salt.

Abstract: The present invention provides a process for producing bicartamide of the formula (4); which comprises Step A comprising reacting Compound (1) of the formula (1); with peroxycarboxylic acid to obtain Compound (2) of the formula (2); Step B comprising reacting said Compound (2) with 4-fluorothiophenol to obtain crude crystals of Compound (3) of the formula (3); dissolving the crude crystals in a solvent and crystallizing to obtain purified crystals of Compound (3), and Step C comprising reacting Compound (3) and percarboxylic acid to obtain bicalutamide, and also provides a method for purifying crystals of Compound (3) which comprises dissolving crude crystals of Compound (3) in a solvent and crystallizing.

Abstract: A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): wherein R1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or —CO2R7 group in which R7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R1 is hydrogen atom and Z is ca

Abstract: The &bgr;-keto ester compound, &bgr;-hydroxy acid compound and acetonide form of a 1,3-diol derivative of the formulas (I), (V) and (VIII) wherein each symbol is as defined in the specification, are useful as a synthetic intermediate for an epothilone derivative being developed as a pharmaceutical agent having an antitumor activity.

Abstract: A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): wherein R1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or —CO2R7 group in which R7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R1 is hydrogen atom and Z is ca

Abstract: A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): 1

Abstract: The &bgr;-keto ester compound, &bgr;-hydroxy acid compound and acetonide form of a 1,3-diol derivative of the formulas (I), (V) and (VIII) 1

Abstract: A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): wherein R1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or —CO2R7 group in which R7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R1 is hydrogen atom and Z is ca

Abstract: A production method of hydrazine derivative having a group of the formula (II) which comprises subjecting a hydrazone derivative having a group of the formula (I) to catalytic reduction and deactivating the reduction catalyst contained in the reaction mixture thereof.

Abstract: A process for preparing tert-butyl 4′-methyl-2-biphenylcarboxylate characterized in that 4′-methyl-2-biphenylcarboxylic acid is reacted with isobutene in the presence of an acid catalyst. According to the present invention, tert-butyl 4′-methyl-2-biphenylcarboxylate having high quality can be conveniently and industrially advantageously prepared in a high yield under mild reaction conditions such as ambient temperatures without complicated procedures or any hazardous solvents.

Abstract: The present invention provides a method for producing a hydrazine derivative of the formula [2]: wherein R1 is alkyl group having 1-12 carbon atoms and the like, R2 is alkyl group having 1-12 carbon atoms and the like, and Ar is phenylene group and the like, from a hydrazone derivative of the formula [1] wherein R1, R2 and Ar are as defined above, in the presence of at least one base selected from the group consisting of an organic base and an inorganic base, and a metal hydrogenating catalyst. By this method, reduction proceeds selectively and a hydrogenolysis reaction (side reaction) can be suppressed.

Abstract: The present invention provides a method for producing a hydrazine derivative of the formula [2]: 1

Abstract: A process for preparing a tert-alkyl carboxylic acid ester represented by the formula (III): wherein R1 is an organic group; and each of R2 and R3 is independently an alkyl group having 1 to 4 carbon atoms, comprising reacting a carboxylic acid represented by the formula (I): R1—COOH  (I) wherein R1 is as defined above, with a vinylidene compound represented by the formula (II): wherein R2 and R3 are as defined above, in the presence of a phosphorus halide. The tert-alkyl carboxylic acid ester can be used as intermediates for pharmaceuticals such as antibiotics.

Abstract: A series of compounds capable of deriving an intermediate for the production of compound (A) of the following formula, which is an anti-HIV drug, and a production method thereof. To be specific, 4-(pyridin-2-yl)benzaldehyde hydrazone, a production method of this compound, and a production method from this compound to N-(tert-butoxycarbonyl)-N′-[4-(pyridin-2-yl)phenylmethylidene]hydrazine. In addition, a salt of 2-(4-bromomethylphenyl)pyridine, 2-(4-dibromomethylphenyl)pyridine and a salt thereof, production methods of these compounds, and production methods to derive 4-(pyridin-2-yl)benzaldehyde which is a production intermediate for 4-(pyridin-2-yl)benzaldehyde hydrazone from these compounds.

Abstract: A series of compounds capable of deriving an intermediate for the production of a compound (A) of the following formula, which is an anti-HIV drug, and a production method thereof. To be specific, 4-(pyridin-2-yl)benzaldehyde hydrazone, a production method of this compound, and a production method from this compound to N-(tert-butoxycarbonyl)-N′-[4-(pyridin-2-yl)phenylmethylidene]hydrazine. In addition, a salt of 2-(4-bromomethylphenyl)pyridine, 2-(4-dibromomethylphenyl)pyridine and a salt thereof, production methods of these compounds, and production methods to derive 4-(pyridin-2-yl)benzaldehyde which is a production intermediate for 4-(pyridin-2-yl)benzaldehyde hydrazone from these compounds.

Abstract: A series of compounds capable of deriving an intermediate for the production of a compound (A) of the following formula, ##STR1## which is an anti-HIV drug, and a production method thereof. To be specific, 4-(pyridin-2-yl)benzaldehyde hydrazone, a production method of this compound, and a production method from this compound to N-(tert-butoxycarbonyl)-N'-[4-(pyridin-2-yl)phenylmethyhidene]hydrazine. In addition, a salt of 2-(4-bromomethylphenyl)pyridine, 2-(4-dibromomethylphenyl)pyridine and a salt thereof, production methods of these compounds, and production methods to derive 4-(pyridin-2-yl)benzaldehyde which is a production intermediate for 4-(pyridin-2-yl)benzaldehyde hydrazone from these compounds.

Abstract: A method of producing a 2-(p-alkylphenyl)pyridine compound economically, easily and industrially, which comprises adding manganese dioxide and trimethylchlorosilane, or adding manganese chloride to an organic ether solvent, and reacting p-alkylphenylmagnesium halide and 2-halopyridine in the obtained organic ether solvent.